Journal
TETRAHEDRON
Volume 68, Issue 14, Pages 2943-2949Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.02.040
Keywords
Janus dendrimer; Amphiphilic; Bone-targeting; Drug delivery
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In this paper, we synthesized a range of amphiphilic Janus dendrimers, which consisted of acidic amino acid and naproxen molecules as the peripheral groups, as novel potential bone-targeting dendritic drug delivery. These dendrimers take advantage of a dendritic display to carry multiple drug molecules and targeting moieties simultaneously. All of the dendrimers exhibited more than 80% binding rates to hydroxyapatite (HAP), especially the [G(2)]-dendrimers (2a and 2b) showed dramatic binding rates (>95%). Moreover, the solubility of naproxen was remarkably enhanced by the dendritic drug delivery system, especially the naproxen concentration of 2b achieved 5.37 mg/ml, which is more than 28-fold over that of native drug. Furthermore, cell viability studies showed that all the dendrimers exhibited no significant cytotoxicity against HEK293 cells. These results provided an effective entry to the development of new bone-targeting drugs. (C) 2012 Elsevier Ltd. All rights reserved.
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